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Flow processing for API production in South Africa: case study towards the synthesis of emtricitabine

corresponding

DEVENDER MANDALA, SRAVANTHI CHADA, PAUL WATTS*
*Corresponding author
Nelson Mandela University, University Way, Port Elizabeth, South Africa

Abstract

We report the optimization and continuous flow synthesis to Emtricitabine, an antiretroviral drug used mainly in highly active antiretroviral therapy (HAART) for the treatment of HIV/AIDS and hepatitis B. Yields for the four step synthesis were improved in the flow synthesis as compared to batch protocol. The overall yield was 39% in 99.75% chiral purity.


INTRODUCTION

South Africa has a number of formulation companies; however all of the active pharmaceutical ingredients (APIs) are imported, principally from India and China.  In an attempt to circumvent this challenge, Nelson Mandela University is working to provide a step change in pharmaceutical manufacturing technology that will increase the local availability and affordability of APIs, with a particular emphasis on South Africa and other developing countries within Africa in the first instance.

Regarding AIDS for example, if more people could receive treatment by reducing the cost of drugs, the number of deaths in South Africa could be massively reduced.  Although the situation has improved through the availability of generics supported through charitable donations in some instances; these medicines can still be expensive, as greater than 70% of generics costs are the API.  The three major drivers behind the cost of the API are CAPEX, labour costs and raw materials. Although it has been observed that labour ...